Bupropion

The Basics

What is Bupropion?

Mostly used to treat major depressive disorder and to support stopping smoking.

Brand names for Bupropion

Aplenzin, Budeprion Sr, Budeprion Xl, Buproban, Forfivo Xl, Wellbutrin, Wellbutrin Sr, Wellbutrin Xl Zyban

How Bupropion is classified

Antidepressive Agents, Antidepressive Agents (Second-Generation), Anti-Obesity Agents

Bupropion During Pregnancy

Bupropion pregnancy category

Category CNote that the FDA has deprecated the use of pregnancy categories, so for some medications, this information isn’t available. We still think it’s useful to list historical info, however, given what a common proxy this has been in the past.

What we know about taking Bupropion while pregnant

Can you take bupropion while pregnant? Data from epidemiological studies including pregnant women exposed to bupropion in the first trimester indicate no increased risk of congenital malformations. All pregnancies regardless of drug exposure have a background rate of 2% to 4% for major malformations and 15% to 20% for pregnancy loss. No clear evidence of teratogenic activity was found in reproductive developmental studies conducted in rats and rabbits. However, in rabbits, slightly increased incidences of fetal malformations and skeletal variations were observed at doses approximately equal to the maximum recommended human dose (MRHD) and greater and decreased fetal weights were seen at doses twice the MRHD and greater. APLENZIN should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Clinical Considerations Consider the risk of untreated depression when discontinuing or changing treatment with antidepressant medications during pregnancy and postpartum.

Taking Bupropion While Breastfeeding

What are recommendations for lactation if you're taking Bupropion?

Limited information indicates that maternal bupropion doses of up to 300 mg daily produce low levels in breastmilk and would not be expected to cause any adverse effects in breastfed infants. However, there is little reported use in breastfed newborn infants and case reports of a possible seizure in partially breastfed 6-month-olds. If bupropion is required by a nursing mother, it is not a reason to discontinue breastfeeding. However, another drug may be preferred, especially while nursing a newborn or preterm infant. Infants exposed to bupropion and an SSRI through breastfeeding should be closely monitored for vomiting, diarrhea, jitteriness, or sedation and possibly measurement of serum levels to rule out toxicity if there is a concern.

Maternal / infant drug levels

Bupropion is metabolized to 3 metabolites (hydroxybupropion, erythrohydroxybupropion, threohydroxybupropion) with the antidepressant activity of each considered to be about 50% of bupropion’s.[1] Maternal Levels: A mother who was 14 months postpartum was taking bupropion 100 mg three times daily. Milk samples were obtained before and at 1, 2, 4 and 6 hours after the first daily dose of 100 mg. Peak bupropion levels of 181 and 189 mcg/L occurred at 1 and 2 hours after the dose, respectively. A peak hydroxybupropion level of 132 mcg/L occurred in milk 2 hours after the dose and peak threohydroxybupropion levels of 443 and 442 mcg/L occurred at 1 and 2 hours after the dose, respectively.[2]Ten women who were an average of 12.5 months postpartum and who did not nurse their infants after the start of bupropion therapy took sustained-release bupropion 150 mg daily for 3 days, then 300 mg daily for 4 days. On the seventh day, breastmilk levels of the drug and metabolites were measured at a median 2.5 hours (range 1 to 12 hours) after the last dose. Breastmilk levels were as follows: bupropion 45.2 mcg/L (range 4 to 168 mcg/L); hydroxybupropion 104.6 mcg/L (range 9 to 242 mcg/L); erythrohydroxybupropion 72.1 mcg/L (range 25.4 to 143 mcg/L); and threohydroxybupropion 459 mcg/L (range 193 to 1052 mcg/L). There was no correlation between the amount of these drugs excreted in milk and maternal or infant age, maternal body mass or breastfeeding frequency prior to the study. The authors estimated that an exclusively breastfed infant would receive an average of 0.2% of the maternal weight-adjusted dosage of bupropion and an average of 2% of the maternal weight-adjusted dosage of bupropion plus metabolites with this maternal dosage regimen.[3]Four women were taking bupropion SR 150 mg or 300 mg for depression or smoking cessation. Maternal milk and serum concentrations were measured before a dose at steady-state and 2 hours after the dose; 2 women had samples taken on 2 separate occasions. Milk bupropion concentrations standardized to a 150 mg dose averaged 64.1 mcg/L (range <10 to 120 mcg/L); metabolites were not measured. The average infant dose (normalized to a 150 mg maternal dose) was estimated to be 21.5 mcg/day (range 5.1 to 31.1 mcg/day) which averaged 5.1% (range 1.4 to 10.6%) of the maternal weight-adjusted dosage.[4]The mother of a 6.5-month-old had been taking escitalopram 10 mg daily since birth and had begun extended-release bupropion 150 mg daily 3 weeks earlier. Stored milk samples from between 6 and 6.25 months postpartum contained bupropion in concentrations ranging from 15.8 mcg/L to 24.4 mcg/L and hydroxybupropion in concentrations ranging from 46 mcg/L to 87 mcg/L.[5] Infant Levels: Bupropion and its metabolites were undetectable (<5 mcg/L for buproion and <20 mcg/L for its metabolites) in one 14-month-old infant 3.7 hours after nursing and 9.5 hours after the mother’s last dose. The infant was nursing twice daily and his mother was taking 100 mg three times a day.[2]One 15-week postpartum mother was taking immediate-release bupropion 75 mg twice daily. After 2 weeks of therapy and full breastfeeding, serum levels of bupropion (<5 mcg/L) and hydroxybupropion (<100 mcg/L) were undetectable in her infant 2 hours after nursing and after the mother’s dose. Another mother who was 29-weeks postpartum was taking sustained-release bupropion 150 mg daily. After 10.5 weeks of therapy and approximately 80% breastfeeding, serum levels of bupropion (<10 mcg/L) and hydroxybupropion (<200 mcg/L) were undetectable in her infant 3.25 hours after nursing and after the mother’s dose.[6]Three breastfed infants ranging in age from 14 to 56 days whose mothers were taking bupropion 150 or 300 mg of bupropion SR had their urine collected 2 hours after a maternal dose; 1 infant had urine collected on 2 occasions. Only one of the infants’ urine samples had detectable amounts (>10 mcg/L) of bupropion at 41 mcg/L; metabolites were not measured.[4]The mother of a 6.5-month-old had been taking escitalopram 10 mg daily since birth and had begun extended-release bupropion 150 mg daily 3 weeks earlier. Her baby was partially breastfed, receiving pumped breastmilk, formula and solid foods. At 6.5 months of age, after having been breastfed 8 hours after the mother’s morning dose of bupropion, the infant was admitted to the emergency department with a seizure and vomiting. The infant’s serum at this time contained a detectable, but non-quantifiable level of bupropion (<4.8 mcg/L) and a serum hydroxybupropion level of 11.2 mcg/L. The following morning the infant’s serum hydroxybupropion level was 17.1 mcg/L.[5]

Possible effects of Bupropion on milk supply

A 34-year-old non-pregnant woman diagnosed with depression was started on bupropion 150 mg daily. During the second week of therapy, she presented with galactorrhea and an elevated serum prolactin level of 98 mcg/L. A cranial MRI found no abnormalities. Bupropion was discontinued and the galactorrhea disappeared in 2 days. One week later, her serum prolactin level was 3 mcg/L. Fluoxetine 20 mg daily was started and continued for 4 months with no signs of galactorrhea.[12]An observational study looked at outcomes of 2859 women who took an antidepressant during the 2 years prior to pregnancy. Compared to women who did not take an antidepressant during pregnancy, mothers who took an antidepressant during all 3 trimesters of pregnancy were 37% less likely to be breastfeeding upon hospital discharge. Mothers who took an antidepressant only during the third trimester were 75% less likely to be breastfeeding at discharge. Those who took an antidepressant only during the first and second trimesters did not have a reduced likelihood of breastfeeding at discharge.[13] The antidepressants used by the mothers were not specified.A retrospective cohort study of hospital electronic medical records from 2001 to 2008 compared women who had been dispensed an antidepressant during late gestation (n = 575) to those who had a psychiatric illness but did not receive an antidepressant (n = 1552) and mothers who did not have a psychiatric diagnosis (n = 30,535). Women who received an antidepressant were 37% less likely to be breastfeeding at discharge than women without a psychiatric diagnosis, but no less likely to be breastfeeding than untreated mothers with a psychiatric diagnosis.[14] None of the mothers were taking bupropion.

Possible alternatives to Bupropion

Nortriptyline, Paroxetine, Sertraline.